Lans Dxr

Uses

Stimulation of gut motility in-

• Non-ulcer dyspepsia
• Oesophageal reflux, reflux oesophagitis and gastritis
• Diabetic gastroparesis
• Functional dyspepsia
• Speeding barium transit in follow through radiological studies

Prevention and symptomatic relief of acute nausea and vomiting from any cause including cytotoxic therapy, radiotherapy and antiparkinsonism therapy.

In the prophylactic treatment of migraine.

Lansoprazole is used for:

• Short term treatment of active duodenal ulcer
• Maintenance of healed duodenal ulcers
• Short term treatment of active benign gastric ulcers
• Short term treatment of active erosive esophagitis
• Maintenance of healing of erosive esophagitis
• Pathological hypersecretory conditions including Zollinger- Ellison Syndrome
• H. pylori eradication to reduce the risk of duodenal ulcer recurrence

Lans Dxr is also used to associated treatment for these conditions: Diabetic Gastroparesis, Dyspepsia, Erosive Esophagitis, Gastrointestinal Symptoms, Non-erosive Reflux Esophagitis Disease (NERD), Upper gastrointestinal motility disordersGastro-esophageal Reflux Disease (GERD), Gastrointestinal Bleeding, Helicobacter Pylori Infection, Peptic Ulcer Disease, Hypersecretory conditions

How Lans Dxr works

Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which - among others - regulates nausea and vomiting

As a PPI, lansoprazole is a prodrug and requires protonation via an acidic environment to become activated. Once protonated, lansoprazole is able to react with cysteine residues, specifically Cys813 and Cys321, on parietal H+,K+-ATPase resulting in stable disulfides. PPI's in general are able to provide prolonged inhibition of acid secretion due to their ability to bind covalently to their targets.

Dosage

Lans Dxr dosage

Adults: 10 - 20 mg every 4 - 8 hours daily

Children: 0.2 - 0.4 mg/kg every 4 - 8 hours daily.

Domperidone tablet and suspension should be taken 15 - 30 minutes before a meal. For acute nausea and vomiting, maximum period of treatment is 12 weeks.

Benign gastric ulcer: 30 mg daily in the morning for 8 weeks.

Duodenal ulcer: 30 mg daily in the morning for 4 weeks; maintenance 15 mg.

NSAID-associated duodenal or gastric ulcer: 15-30 mg daily for 4 weeks, followed by a further 4 weeks if not fully healed.

Zollinger-Ellison syndrome (and other hypersecretory conditions): Initially 60 mg once daily adjusted according to response; daily doses of 120 mg or more is given in two divided doses.

Gastroesophageal reflux disease: 30 mg daily in the morning for 4 weeks, followed by a further 4 weeks if not fully healed; maintenance 15-30 mg daily.

Acid-related dyspepsia: 15-30 mg daily in the morning for 2-4 weeks.

Side Effects

Domperidone may produce hyperprolactinemia which may cause galactorrhea & breast enlargement, soreness and reduced libido. It may rarely cause dry mouth, thirst, headache, nervousness, drowsiness, diarrhea, skin rash and itching.

Severe or irreversible adverse effects: The possible induction of carcinoid tumors by profound acid suppression, and a rise in serum gastrin may occur. There is a rise in serum gastrin levels in the first 3 months of treatment, which are then maintained though at a lower level than those found in pernicious anaemia. Long term treatment with a proton pump inhibitor in patients with Helicobacter pylori infection may accelerate the development of atrophic gastritis.

Symptomatic adverse effect: Dose dependent diarrhoea occurs with an incidence of about 4% at 30 mg per day, rising to 8% at 60 mg per day. Headache occurs in 2-3% of treated patients

Toxicity

Side effects include galactorrhea, gynecomastia, or menstrual irregularities.

The most commonly reported adverse events occurring more frequently in lansoprazole treated patients compared to placebo include abdominal pain, constipation, diarrhea, and nausea. There is a case report of toxic epidermal necrolysis (TEN), which is a rare but very serious cutaneous reaction, caused by lansoprazole. The previously healthy patient presented with symptoms of TEN 15 days after starting lansoprazole to manage peptic disease. Although the use of PPI's is rarely associated with TEN, causation should be considered if a patient presents with TEN shortly after newly commencing a PPI.

In a single case report, a patient ingested 600 mg of lansoprazole and did not experience any adverse effects or symptoms of overdose. Overall, lansoprazole is well tolerated with relatively few adverse effects.

Lansoprazole is classified as Pregnancy Category B. Although there are animal studies that suggest lansoprazole does not cause harm to the fetus, there is still a paucity of human data. Hence, lansoprazole should only be administered to pregnant women if other options with more safety data have been exhausted.

It is unknown if lansoprazole is excreted in human breast milk. It is worth mentioning that lansoprazole has been used safely in infants, and is therefore likely safe to use during breastfeeding.

Precaution

Domperidone should be used with absolute caution in case of children because there may be an increased risk of extra-pyramidal reactions in young children because of an incompletely developed blood brain barrier.

Gastric malignancy should be ruled out. Hepatic impairment. Pregnancy and lactation.

Interaction

Domperidone may reduce the hypoprolactinaemic effect of bromocriptine. Anti-muscarinics and opioid analgesics may antagonize the action of Domperidone on gastrointestinal function.

Lansoprazole appears to be a selective inhibitor of the cytochrome P-450 monooxygenase system; there may be an effect on hepatic clearance, but there have been no reports to date of clinically relevant interactions. There is some uncertainty over the effect of Lansoprazole on the oral combined contraceptive pill. Further assessment is currently underway. Physiological changes similar to those found with Omeprazole are likely to take place because of the reduction in gastric acid, which is likely to influence the bacterial colonization of the stomach and duodenum and also vitamin B12 absorption.

Volume of Distribution

The apparent volume of distribution of lansoprazole is 0.4 L/kg.

Elimination Route

The oral bioavailability of lansoprazole is reported to be 80-90% and the peak plasma concentration(Cmax) is achieved about 1.7 hours after oral dosing. Food reduces the absorption of lansoprazole (both Cmax and AUC are reduced by 50-70%); therefore, patients should be instructed to take lansoprazole before meals.

Half Life

7 hours

One source reports the half life of lansoprazole to be 0.9 - 1.6 hours, while another source cites 0.9 - 2.1 hours. The general consensus is that lansoprazole has a short half life and is approximately 2 hours or less. These numbers may be misleading since it suggests that lansoprazole has a short duration of action when in practice, lansoprazole can effectively inhibit acid secretion for ~24 hours due to it's mechanism of action.

Clearance

The reported clearance of lansoprazole is 400-650 mL/min.

Elimination Route

A reported 14-23% of a lansoprazole is eliminated in the urine with this percentage range including both conjugated and unconjugated hydroxylated metabolites.

Pregnancy & Breastfeeding use

Use in pregnancy: The safety of this drug has not been established for pregnant women. So it is not recommended during pregnancy.

Use in lactation: Domperidone may precipitate galactorrhea and improve postnatal lactation, which is secreted in breast milk but in very small quantities insufficient to be considered harmful.

Lansoprazole should be avoided in pregnancy unless there are compelling reasons.

Contraindication

Domperidone is contraindicated to the patients who have hypersensitivity to this drug and in case of neonates.

Lansoprazole is contraindicated in patients with known hypersensitivity to any component of the formulation.

Special Warning

Neonates:There is no relevant human data. The drug is not recommended for use with neonates.

Children: The youngest person to have received Lansoprazole in clinical trials was 13 years old.

The Elderly: No problems have been encoun- tered in clinical use and there has been no increase in adverse drug reaction in the elderly.

Acute Overdose

Overdose has been reported primarily in infants and children. Symptoms of overdosage may include disorientation, somnolence and extrapyramidal reactions. There is no specific antidote to domperidone, but in the event of overdose, the administration of activated charcoal may be useful. Anticholinergics, antiparkinson drugs may be useful in controlling extrapyramidal reactions. The patient should be observed closely and supportive measures employed.

Storage Condition

Store in a cool dry place protected from light. Keep out of reach of children.

Store at 25° C.

Innovators Monograph

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